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Pathways Recommended: Membrane Transporter/Ion Channel
Targets Recommended: GlyT mAChR nAChR

Results for "Acetylcholine Transporters Inhibitors" in MCE Product Catalog:

229

Inhibitors & Agonists

3

Screening Libraries

4

Dye Reagents

1

Biochemical Assay Reagents

10

Peptides

39

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-B0282
    Acetylcholine chloride

    ACh chloride

    Calcium Channel Autophagy Endogenous Metabolite Neurological Disease Cancer
    Acetylcholine chloride (ACh chloride) is a common neurotransmitter found in the central and peripheral nerve system.
  • HY-101086
    Acetylcholine iodide

    ACh iodide

    Others Cancer Neurological Disease
    Acetylcholine iodide (ACh iodide) is a common neurotransmitter found in the central and peripheral nerve system.
  • HY-N7506
    13-Hydroxyisobakuchiol

    Delta3,2-Hydroxylbakuchiol

    Monoamine Transporter Dopamine Transporter Neurological Disease
    Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol), an analog of Bakuchiol (HY-N0235) isolated from Psoralea corylifolia (L.), is a potent monoamine transporter inhibitor. 13-Hydroxyisobakuchiol is more selective for the dopamine transporter (DAT) (IC50=0.58 μM) and norepinephrine transporter (NET) (IC50=0.69 μM) than for the serotonin transporter (SERT) (IC50=312.02 μM). 13-Hydroxyisobakuchiol has the potential for the research of disorders such as Parkinson's disease, depression, and cocaine addiction.
  • HY-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-W010936
    Nitrobenzylthioinosine

    NBMPR

    Adenosine Receptor Neurological Disease
    Nitrobenzylthioinosine is an ENT1 transporter inhibitor that binds to ENT1 transporter with high affinity. Nitrobenzylthioinosine is a photoaffinity probe for adenosine uptake sites in brain. Nitrobenzylthioinosine crosses the blood-brain barrier.
  • HY-136146
    SUVN-911

    nAChR Neurological Disease
    SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity.
  • HY-18728
    STF-31

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-101372A
    Oxotremorine M iodide

    mAChR Neurological Disease
    Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms.
  • HY-N4080
    Cyclobuxine D

    mAChR Inflammation/Immunology
    Cyclobuxine D is a steroidal alkaloid extracted from Buxus microphylla. Cyclobuxine D has a significant bradycardic effect in the rat heart and an inhibitory action on acetylcholine and Ba ++−induced contraction of the longitudinal muscle isolated from the rabbit jejunum.
  • HY-101315
    AHN 1-055 hydrochloride

    3α-Bis-(4-fluorophenyl) Methoxytropane hydrochloride

    Dopamine Transporter Neurological Disease
    AHN 1-055 hydrochloride is a dopamine uptake inhibitor, with an IC50 of 71 nM. AHN 1-055 hydrochloride binds with high affinity to the dopamine transporter (DAT) and may serve as leads for the development of agentia to treat cocaine abuse.
  • HY-B2246A
    D-Carnitine hydrochloride

    (S)-Carnitine hydrochloride

    Endogenous Metabolite Metabolic Disease
    D-Carnitine hydrochloride ((S)-Carnitine Hydrochloride) has been used to study sulfur factor transporter SLC22A4 and carnitine transporter SLC22A5 in ergot. D-Carnitine hydrochloride is also used to get palmitic acid into mitochondria.
  • HY-101190
    Volixibat

    SHP626; LUM002

    Others Metabolic Disease
    Volixibat (SHP626) is a highly selective, minimally absorbed, and competitive apical sodium-dependent bile acid transporter (ASBT) inhibitor. Volixibat has potential for treatment for non-alcoholic steatohepatitis (NASH).
  • HY-119996A
    AR-C141990 hydrochloride

    Monocarboxylate Transporter Inflammation/Immunology
    AR-C141990 hydrochloride is a potent lactate transporters (monocarboxylate transporters; MCTs) inhibitor with pKi values of 7.6, 6.6 for MCT-1 and MCT-2, respectively. AR-C141990 hydrochloride has immunosuppressive properties and inhibits graft versus host response.
  • HY-100234A
    DREADD agonist 21 dihydrochloride

    mAChR Neurological Disease
    DREADD agonist 21 dihydrochloride is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7 nM).
  • HY-100234
    DREADD agonist 21

    mAChR Neurological Disease
    DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7 nM).
  • HY-W011391
    GPNA hydrochloride

    Apoptosis Cancer
    GPNA hydrochloride is a well known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride is a specific glutamine (Gln) transporter ASCT2 inhibitor. GPNA hydrochloride also inhibit Na +-dependent carriers, such as SNAT family (SNAT1/2/4/5), and the Na +-independent leucine transporters LAT1/2. GPNA reversibly induces apoptosis in A549 cells.
  • HY-109043A
    Solriamfetol hydrochloride

    JZP-110 hydrochloride; ADX-N05 hydrochloride; R228060 hydrochloride

    Dopamine Receptor Neurological Disease
    Solriamfetol hydrochloride (JZP-110 hydrochloride) is an orally active and selective dopamine and norepinephrine reuptake inhibitor with IC50s of 2.9 μM and 4.4 μM for dopamine and norepinephrine transporters, respectively. Solriamfetol hydrochloride has robust wake-promoting effects.
  • HY-109043
    Solriamfetol

    JZP-110; ADX-N05; R228060

    Dopamine Receptor Neurological Disease
    Solriamfetol (JZP-110) is an orally active and selective dopamine and norepinephrine reuptake inhibitor with IC50s of 2.9 μM and 4.4 μM for dopamine and norepinephrine transporters, respectively. Solriamfetol has robust wake-promoting effects.
  • HY-110160
    Pozanicline dihydrochloride

    ABT-089 dihydrochloride

    nAChR Neurological Disease
    Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [ 3H]cytisine sites. Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant.
  • HY-P1271
    Catestatin

    nAChR Cardiovascular Disease
    Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
  • HY-107416
    RHC 80267

    U-57908

    Acyltransferase mAChR COX Phospholipase Metabolic Disease Neurological Disease
    RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC50 of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC50 of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC).
  • HY-14563
    VU10010

    mAChR Neurological Disease
    VU10010 is a potent, highly selective and allosteric M4 mAChR potentiator with an EC50 of 400 nM. VU10010 binds to an allosteric site on M4 mAChR and increases affinity for acetylcholine and coupling to G proteins. VU10010 increases carbachol-induced depression of transmission at excitatory but not inhibitory synapses in the hippocampus.
  • HY-P1271A
    Catestatin TFA

    nAChR Cardiovascular Disease
    Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
  • HY-W020468
    Linopirdine

    DuP 996

    Potassium Channel TRP Channel Neurological Disease
    Linopirdine (DuP 996) is an orally active, selective M-type K + current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue.
  • HY-100017
    BAY-876

    GLUT Cancer
    BAY-876 is an orally active and selective glucose transporter 1 (GLUT1) inhibitor with an IC50 of 2 nM. BAY-876 is >130-fold more selective for GLUT1 than GLUT2, GLUT3, and GLUT4. BAY-876 is also a potent blocker of glycolytic metabolism and ovarian cancer growth.
  • HY-N7433
    4,6-O-Ethylidene-α-D-glucose

    Ethylidene-glucose

    GLUT Endogenous Metabolite Metabolic Disease
    4,6-O-ethylidene-α-D-glucose (Ethylidene-glucose), a glucose derivative, is a competitive exofacial binding-site inhibitor on glucose transporter 1 (GLUT1) with a Ki of 12 mM for wild-type 2-deoxy-D-glucose transport.
  • HY-107641
    α-Cyano-4-hydroxycinnamic acid

    α-Cyano-4-hydroxycinnamate

    Monocarboxylate Transporter Metabolic Disease
    α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. α-Cyano-4-hydroxycinnamic acid is used as a matrix to facilitate peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications.
  • HY-17590
    Radafaxine hydrochloride

    GW-353162A; BW-306U

    Monoamine Transporter Neurological Disease
    Radafaxine hydrochloride (GW-353162A) is a DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator.
  • HY-18638
    TCID

    4,5,6,7-Tetrachloroindan-1,3-dione

    Deubiquitinase Neurological Disease
    TCID (4,5,6,7-Tetrachloroindan-1,3-dione) is a potent and selective neuronal ubiquitin C-terminal hydrolase (UCH-L3) inhibitor with an IC50 of 0.6 μM. TCID diminishes glycine transporter GlyT2 ubiquitination in brainstem and spinal cord primary neurons.
  • HY-B0457
    Clomipramine hydrochloride

    Serotonin Transporter Dopamine Receptor Neurological Disease
    Clomipramine hydrochloride is a serotonin transporter (SERT), norepinephrine transporter (NET) and dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively.
  • HY-B1272
    Desipramine hydrochloride

    Dopamine Transporter Serotonin Transporter Neurological Disease Cancer
    Desipramine hydrochloride is an inhibitor of norepinephrine transporter (NET), 5-HT transporter (SERT) and dopamine transporter (DAT) with Kis of 4, 61 and 78,720 nM, respectively.
  • HY-112683
    V-9302

    Others Cancer
    V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5). V-9302 inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells.
  • HY-112683A
    V-9302 hydrochloride

    Others Cancer
    V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5). V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells.
  • HY-16736
    Centanafadine

    EB-1020

    Adrenergic Receptor Dopamine Transporter Serotonin Transporter Neurological Disease Endocrinology
    Centanafadine is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.
  • HY-16736A
    Centanafadine hydrochloride

    EB-1020 hydrochloride

    Adrenergic Receptor Dopamine Transporter Serotonin Transporter Neurological Disease Endocrinology
    Centanafadine (hydrochloride) is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.
  • HY-N0322
    Cholesterol

    Estrogen Receptor/ERR Endogenous Metabolite Metabolic Disease
    Cholesterol is the major sterol in mammals and is makes up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.
  • HY-B0457AS
    Clomipramine D3

    Serotonin Transporter Dopamine Receptor Neurological Disease
    Clomipramine D3 is the deuterium labeled Clomipramine. Clomipramine is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively.
  • HY-B0457S
    Clomipramine D3 hydrochloride

    Serotonin Transporter Dopamine Receptor Neurological Disease
    Clomipramine D3 hydrochloride is a deuterium labeled Clomipramine hydrochloride. Clomipramine hydrochloride is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively.
  • HY-17360
    Tiotropium Bromide

    BA679 BR

    mAChR Neurological Disease
    Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
  • HY-B1547A
    Benzetimide hydrochloride

    R4929

    mAChR Neurological Disease
    Benzetimide hydrochloride is a muscarinic acetylcholine receptor antagonist.
  • HY-U00067
    Ambutonium bromide

    BL700

    mAChR Inflammation/Immunology
    Ambutonium bromide is an acetylcholine antagonist.
  • HY-B0590A
    Tetrabenazine Racemate

    Ro 1-9569 Racemate

    Monoamine Transporter Neurological Disease
    Tetrabenazine Racemate (Ro 1-9569 Racemate) is a selective and reversible inhibitor of vesicular monoamine transporter-2 (VMAT-2).
  • HY-B2070
    Methylbenactyzium Bromide

    mAChR Inflammation/Immunology
    Methylbenactyzium Bromide is a muscarinic acetylcholine receptor (mAChR) inhibitor.
  • HY-107794
    Clodronate disodium tetrahydrate

    Disodium clodronate tetrahydrate

    Others Inflammation/Immunology Neurological Disease
    Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl - competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC50 of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-B0327A
    Irsogladine maleate

    Dicloguamine maleate; MN1695

    mAChR Phosphodiesterase (PDE) Inflammation/Immunology
    Irsogladine is a PDE4 inhibitor and muscarinic acetylcholine receptor binder.
  • HY-B0327
    Irsogladine

    Dicloguamine

    mAChR Phosphodiesterase (PDE) Inflammation/Immunology
    Irsogladine is a PDE4 inhibitor and muscarinic acetylcholine receptor binder.
  • HY-114381
    GT 949

    EAAT2 Neurological Disease
    GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM.
  • HY-B0489
    Arecoline hydrobromide

    Arecoline bromide

    mAChR Neurological Disease
    Arecoline hydrobromide (Arecoline bromide) is a muscarinic acetylcholine receptor agonist.
  • HY-U00316
    Vinconate

    Chanodesethylapovinc​amine

    mAChR Neurological Disease
    Vinconate is an indolonaphthyridine derivative and can stimulate the muscariic acetylcholine receptor.
  • HY-16423
    Rapacuronium bromide

    Org 9487

    mAChR Neurological Disease
    Rapacuronium bromide is an allosteric modulator of muscarinic acetylcholine receptor (mAChR).
  • HY-101743
    Elucaine

    mAChR Inflammation/Immunology
    Elucaine is a muscarinic acetylcholine receptor antagonist with anti-ulcerative activity.
  • HY-101036
    Choline bitartrate

    mAChR Neurological Disease
    Choline (bitartrate) is an essential nutrient, often associated with the B vitamins but not yet officially defined as a B vitamin. Choline (bitartrate) plays an important role in synthesis of the neurotransmitter acetylcholine.
  • HY-B0962A
    Piperidolate

    mAChR Neurological Disease
    Piperidolate is an antimuscarinic, inhibits intestinal cramp induced by acetylcholine (rats and dogs).
  • HY-B0962
    Piperidolate hydrochloride

    mAChR Neurological Disease
    Piperidolate hydrochloride is an antimuscarinic, inhibits intestinal cramp induced by acetylcholine (rats and dogs).
  • HY-B1490
    Imipramine hydrochloride

    Serotonin Transporter Neurological Disease
    Imipramine hydrochloride inhibits serotonin transporter with an IC50 value of 32 nM in vitro.
  • HY-N0480A
    Reserpine hydrochloride

    Monoamine Transporter Cancer Neurological Disease
    Reserpine hydrochloride is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).
  • HY-N0480
    Reserpine

    Monoamine Transporter Autophagy Neurological Disease Cancer
    Reserpine is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-B0942
    Benzethonium chloride

    nAChR Neurological Disease
    Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes.
  • HY-10716A
    PF-03463275

    GlyT Neurological Disease
    PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research.
  • HY-19887
    Tilapertin

    AMG747

    GlyT Neurological Disease
    Tilapertin is an oral inhibitor of glycine transporter type-1 (GlyT1).
  • HY-100152
    Beperidium iodide

    SX 810

    mAChR Inflammation/Immunology
    Beperidium iodide shows a competitive antagonistic effect against acetylcholine receptor with a pA2 of 7.93.
  • HY-B1205A
    Atropine sulfate

    Sulfatropinol

    mAChR Neurological Disease
    Atropine sulfate (Sulfatropinol) is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist.
  • HY-17530
    Aldicarb sulfone

    AChE Others
    Aldicarb sulfone(Temik sulfone) is a carbamate insecticide; is a cholinesterase inhibitor which prevents the breakdown of acetylcholine in the synapse.
  • HY-N2332A
    Methyllycaconitine citrate

    MLA

    nAChR Infection
    Methyllycaconitine citrate is a specific antagonist of α7 neuronal nicotinic acetylcholine receptor (α7nAChR).
  • HY-110176
    ASP2535

    GlyT Neurological Disease
    ASP2535 is a potent, orally bioavailable, selective, brain permeable and centrally-active glycine transporter-1 (GlyT1) inhibitor. ASP2535 can improve cognitive impairment in animal models of schizophrenia and Alzheimer's disease.
  • HY-N0443
    N-Methylcytisine

    Caulophylline

    nAChR Inflammation/Immunology
    N-Methylcytisine (Caulophylline), a tricyclic quinolizidine alkaloid, exerts hypoglycaemic, analgesic and anti-inflammatory activities. N-methylcytisine is a selective ligand of nicotinic receptors of acetylcholine in the central nervous system and has a high affinity (Kd = 50 nM) to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia.
  • HY-15430A
    Encenicline hydrochloride

    EVP-6124 (hydrochloride)

    nAChR Neurological Disease
    Encenicline hydrochloride (EVP-6124 hydrochloride) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).
  • HY-15430
    Encenicline

    EVP-6124

    nAChR Neurological Disease
    Encenicline (EVP-6124) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).
  • HY-B0726
    Pilocarpine Hydrochloride

    mAChR Neurological Disease
    Pilocarpine Hydrochloride is a selective M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.
  • HY-128723
    Dapagliflozin impurity

    Others Others
    Dapagliflozin impurity is an enantiomer of Dapagliflozin which is a sodium-glucose transporter 2 inhibitor.
  • HY-107675
    Desformylflustrabromine hydrochloride

    Deformylflustrabromine hydrochloride; dFBr hydrochloride

    nAChR Neurological Disease
    Desformylflustrabromine hydrochloride is a selective agonist of α4β2 neuronal nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.48.
  • HY-14774
    Monepantel

    AAD1566

    nAChR Cancer
    Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
  • HY-B1006
    Pilocarpine nitrate

    mAChR Neurological Disease
    Pilocarpine nitrate is a selective M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.
  • HY-13596
    Cisatracurium besylate

    51W89

    nAChR Autophagy Neurological Disease Cancer
    Cisatracurium besylate (51W89) is a nondepolarizing neuromuscular blocking agent, antagonizing the action of acetylcholine by inhibiting neuromuscular transmission.
  • HY-B0827
    Dinotefuran

    MTI-446

    Parasite nAChR Infection
    Dinotefuran is an insecticide of the neonicotinoid class, its mechanism of action involves disruption of the insect's nervous system by inhibiting nicotinic acetylcholine receptors.
  • HY-B0882
    Edrophonium chloride

    AChE Neurological Disease
    Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
  • HY-128380
    Dibenamine hydrochloride

    N-​(2-​Chloroethyl)​dibenzylamine hydrochloride

    Adrenergic Receptor Metabolic Disease
    Dibenamine hydrochloride is a competitive and irreversible adrenergic blocking agent and is known to modify the pharmacological effects of epinephrine. Dibenamine hydrochloride cause a significant increase in the rate of destruction of I-epinephrine in the mouse.
  • HY-10010
    Ko 143

    BCRP Cancer
    Ko 143 is a potent and selective ATP-binding cassette subfamily G member 2 (ABCG2/BCRP) inhibitor. Ko 143 displays >200-fold selectivity over P-gp and MRP-1 transporters.
  • HY-19373
    RWJ-445167

    3DP-10017

    Thrombin Factor Xa Cardiovascular Disease
    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  • HY-16787
    ICA-121431

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • HY-N7004
    Arborine

    mAChR Cardiovascular Disease
    Arborine, isolated from Glycosmis arborea, inhibits the peripheral action of acetylcholine and induces a fall in blood pressure.
  • HY-14564A
    GTS-21 dihydrochloride

    DMXB-A; DMBX-anabaseine

    nAChR Inflammation/Immunology
    GTS-21 dihydrochloride is a selective α7 nicotinic acetylcholine receptor agonist, has recently been established as a promising treatment for inflammation.
  • HY-N3610
    Coclaurine

    nAChR Neurological Disease
    Coclaurine is a class of tetrahydroisoquinoline alkaloids isolated from Sarcopetalum harveyanum. Coclaurine is a nicotinic acetylcholine receptor (nAChRs) antagonist.
  • HY-101334
    MPDC

    GlyT Neurological Disease
    MPDC is a potent and competitive inhibitor of the Na+-dependent high-affinity glutamate transporter in forebrain synaptosomes.
  • HY-B0394
    Atropine sulfate monohydrate

    Atropine sulfate hydrate

    mAChR Autophagy Neurological Disease
    Atropine sulfate monohydrate (Atropine sulfate hydrate) is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect.
  • HY-B0106
    Levetiracetam

    UCB L059

    mAChR Neurological Disease
    Levetiracetam (UCB L059) is a selective M2 muscarinic acetylcholine receptors (mAChR) inhibitor. Antiepileptic agent.
  • HY-B0034
    Donepezil Hydrochloride

    E2020

    AChE Neurological Disease
    Donepezil (Hydrochloride) (E-2020) is a noncompetitive acetylcholinesterase inhibitor, which can readily cross the blood brain barrier and increases the concentration of cortical acetylcholine.
  • HY-12157
    VU 0238429

    mAChR Others
    VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
  • HY-14261
    Vilazodone Hydrochloride

    EMD 68843 Hydrochloride; SB659746A Hydrochloride

    5-HT Receptor Serotonin Transporter Neurological Disease
    Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
  • HY-15793
    NBI-98782

    (+)-DTBZ; (+)-α-Dihydrotetrabenazine; (+)-α-DHTBZ

    Monoamine Transporter Neurological Disease
    NBI-98782(alpha-dihydrotetrabenazine) is a vesicular monoamine transporter (VMAT2) inhibtior with an Ki value of 0.97 nM.
  • HY-12850
    Dasotraline

    SEP 225289

    Dopamine Transporter Serotonin Transporter Neurological Disease
    Dasotraline is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
  • HY-10914
    UCPH-101

    Others Neurological Disease
    UCPH-101 is an excitatory amino acid transporter subtype 1 (EAAT1) inhibitor with an IC50 of 0.66 μM.
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

    (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-107526
    NFPS

    GlyT Neurological Disease
    NFPS is a selective, non-competitive glycine transporter-1 (GlyT1) inhibitor with IC50s of 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively. NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion.
  • HY-B0823
    Acetamiprid

    nAChR Neurological Disease
    Acetamiprid is a neonicotinoid insecticide used worldwide. Acetamiprid is a nicotinic acetylcholine receptor (nAChR) agonist, and is shown to be associated with neuromuscular and reproductive disorders.
  • HY-100390
    (S)-ML753286

    BCRP Cancer
    (S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
  • HY-B1110
    Nomifensine

    (±)-Nomifensin

    Dopamine Receptor Neurological Disease
    Nomifensine is a norepinephrine-dopamine reuptake inhibitor, increases the amount of synaptic norepinephrine and dopamine available to receptors by blocking the dopamine and norepinephrine reuptake transporters.
  • HY-124738
    BI 01383298

    Sodium Channel Metabolic Disease
    BI 01383298 is a potent inhibitor of the sodium-citrate co-transporter (SLC13A5) that is highly expressed in the liver.
  • HY-B0590S1
    (+)-Tetrabenazine D6

    Monoamine Transporter
    (+)-Tetrabenazine D6 is the deuterium labeled (+)-Tetrabenazine. (+)-Tetrabenazine is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2).
  • HY-124540B
    (Rac)-ABT-202 dihydrochloride

    nAChR Neurological Disease
    (Rac)-ABT-202 dihydrochloride is a racemate of ABT-202. ABT-202 is an agonist of nicotinic acetylcholine receptors (nAChRs) and can be used as an analgesic.
  • HY-N2338
    Cholesterol myristate

    Cholesteryl myristate; Cholesteryl tetradecanoate

    nAChR GABA Receptor Potassium Channel Endogenous Metabolite Cancer
    Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAA receptor, and the inward-rectifier potassium ion channel.
  • HY-101037
    Sarcosine

    N-Methylglycine; Sarcosin

    Endogenous Metabolite GlyT Cancer
    Sarcosine is a glycine transporter type 1 (GlyT) inhibitor and an N-methyl-D-aspartate (NMDA) receptor co-agonist at the glycine binding site.
  • HY-13248
    AR-C155858

    Monocarboxylate Transporter Others
    AR-C155858 is a selective monocarboxylate transporter MCT1 and MCT2 inhibitor with Kis of 2.3 nM and 10 nM, respectively.
  • HY-112843
    CNT2 inhibitor-1

    Others Others
    CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC50 of 640 nM for hCNT2.
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-B0602
    Desvenlafaxine

    O-Desmethylvenlafaxine

    Serotonin Transporter Neurological Disease
    Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter.
  • HY-B0106A
    Etiracetam

    UCB 6474

    Calcium Channel Neurological Disease
    Etiracetam (UCB 6474) is an acetylcholine agonist and a nootropic drug of the racetam family. Less active than its S-enantiomer Levetiracetam (UCB L059).
  • HY-14824
    Sofiniclin

    ABT 894

    nAChR Neurological Disease
    Sofiniclin (ABT 894), an agonist of nicotinic acetylcholine receptor (nAChR), is used as a potential non-stimulant research for attention-deficit/hyperactivity disorder (ADHD).
  • HY-107522
    DL-TBOA

    EAAT2 Neurological Disease
    DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA inhibits the uptake of [ 14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively.
  • HY-B0937
    Amprolium

    Parasite Infection
    Amprolium is a coccidiostat used in poultry, is a thiamine analogue and blocks the thiamine transporter of Eimeria species by blocking thiamine uptake it prevents carbohydrate synthesis.
  • HY-B0937A
    Amprolium hydrochloride

    Parasite Infection
    Amprolium hydrochloride is a coccidiostat used in poultry, is a thiamine analogue and blocks the thiamine transporter of Eimeria species by blocking thiamine uptake it prevents carbohydrate synthesis.
  • HY-12850A
    Dasotraline hydrochloride

    SEP-225289 hydrochloride

    Serotonin Transporter Dopamine Transporter Neurological Disease
    Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
  • HY-B0602A
    Desvenlafaxine succinate hydrate

    O-Desmethylvenlafaxine succinate hydrate

    Serotonin Transporter Neurological Disease
    Desvenlafaxine succinate hydrate, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine succinate hydrate shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter.
  • HY-101381
    Otenzepad

    AF-DX 116

    mAChR Metabolic Disease Neurological Disease
    Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively.
  • HY-100809
    Guvacine hydrochloride

    GABA Receptor Neurological Disease
    Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and dispalys modest selectivity for cloned GABA transporters with IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).
  • HY-19331
    WZB117

    GLUT Cancer
    WZB117 is a glucose transporter 1 (Glut1) inhibitor, which downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo.
  • HY-15258A
    Lesinurad sodium

    RDEA-594 sodium

    URAT1 Metabolic Disease
    Lesinurad sodium is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 µM, respectively.
  • HY-15258
    Lesinurad

    RDEA594

    URAT1 Metabolic Disease
    Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 µM, respectively.
  • HY-N1064
    Xanthoplanine

    nAChR Neurological Disease
    Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC50 ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC50 values of 9 μM (alpha7) and 5 μM (alpha4beta2).
  • HY-12560D
    PNU-282987 S enantiomer free base

    nAChR Others
    PNU-282987 S enantiomer free base is the S-enantiomer of PNU-282987 free base. PNU-282987 is an α7 nicotinic acetylcholine receptor (α7 nAChR) agonist.
  • HY-12149
    A-867744

    nAChR Autophagy Neurological Disease
    A-867744 is a highly potent and selective type II positive allosteric modulator (PAM) of the alpha7 nicotinic acetylcholine receptors (nAChR) with an EC50 of 1.0 μM.
  • HY-12641
    Pyrantel tartrate

    Parasite Antibiotic Infection
    Pyrantel tartrate is an antinematodal thiophene; nicotinic receptor agonist and can elicit spastic muscle paralysis in parasitic worms due to prolonged activation of the excitatory nicotinic acetylcholine (nACh) receptors on body wall muscle.
  • HY-117506B
    SBFI-26

    FABP Inflammation/Immunology Neurological Disease
    SBFI-26 is a selective and competitive inhibitor of fatty acid binding proteins FABP5 and FABP7, with Kis of 0.9 µM and 0.4 µM for FABP5 and FABP7, respectively. SBFI-26 produces anti-nociceptive and anti-inflammatory effects.
  • HY-W013093
    Uridine triphosphate trisodium salt

    UTP trisodium salt; Uridine 5'-triphosphate trisodium salt

    Others Cancer Inflammation/Immunology Cardiovascular Disease
    Uridine triphosphate trisodium salt is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
  • HY-135813
    LtaS-IN-1

    Bacterial Infection
    LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
  • HY-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-B0820
    Nitenpyram

    nAChR Neurological Disease
    Nitenpyram is a calss of neonicotinoid and an insect nicotinic acetylcholine receptor (nAChR) agonist with an IC50 of 14 nM. Nitenpyram is an oral fast-acting insecticide used to suppress sucking insects on companion animals.
  • HY-100806
    Kynurenic acid

    Quinurenic acid

    iGluR Endogenous Metabolite Apoptosis Inflammation/Immunology Neurological Disease Endocrinology
    Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
  • HY-107512
    Kynurenic acid sodium

    iGluR Apoptosis Inflammation/Immunology Neurological Disease Endocrinology
    Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.
  • HY-110241
    Dianicline dihydrochloride

    nAChR Neurological Disease
    Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of drugs that includes varenicline and cytisine for smoking cessation. Dianicline dihydrochloride increases cessation rates in a dose-dependent manner.
  • HY-128574
    GLUT4 activator 1

    GLUT Metabolic Disease
    GLUT4 activator 1 (Compound 26b) is a potent glucose transporter type 4 (GLUT4) translocation activator with an EC50 of 0.14 μM.
  • HY-B1205
    Atropine

    Tropine tropate; DL-Hyoscyamine

    mAChR Endogenous Metabolite Neurological Disease
    Atropine (Tropine tropate) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist, with anti-myopia effect. Atropine blocks the inhibitory effect of ACh on heart rate and contractility, potentially also leading to tachyarrhythmias.
  • HY-107625A
    SNAP 94847 hydrochloride

    MCHR1 (GPR24) Neurological Disease
    SNAP 94847 hydrochloride is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 hydrochloride binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.
  • HY-107625
    SNAP 94847

    MCHR1 (GPR24) Neurological Disease Endocrinology
    SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.
  • HY-107372
    Uridine triphosphate

    UTP; Uridine 5'-triphosphate

    Endogenous Metabolite Cancer Inflammation/Immunology Cardiovascular Disease
    Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
  • HY-112807
    SGLT inhibitor-1

    SGLT Metabolic Disease
    SGLT inhibitor-1 is a potent dual inhibitor of sodium glucose co-transporter proteins (SGLTs), inhibits hSGLT1 and hSGLT2 with IC50s of 43 nM and 9 nM, respectively.
  • HY-112209
    VU0467154

    mAChR Neurological Disease
    VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
  • HY-P1269
    α-Conotoxin AuIB

    nAChR Neurological Disease
    α-Conotoxin AuIB, a potent and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist, blocks α3β4 nAChRs expressed in Xenopus oocytes with an IC50 of 0.75 μM.
  • HY-114309
    URAT1 inhibitor 1

    URAT1 Inflammation/Immunology
    URAT1 inhibitor 1 (1g) is a uric acid transporter 1 (URAT1) inhibitor, with an IC50 of 32 nM. URAT1 inhibitor 1 has potential to treat hyperuricemia associated with gout.
  • HY-126301
    DMT1 blocker 1

    Others Inflammation/Immunology
    DMT1 blocker 1 is a blocker of divalent metal transporter 1 (DMT1) with an IC50 of 0.64 μM, is expected to block iron uptake by enterocytes in vivo.
  • HY-12560A
    PNU-282987

    nAChR Neurological Disease
    PNU-282987 is a selective α7 nicotinic acetylcholine receptor(α7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM).
  • HY-N7247
    Thiochrome

    mAChR Metabolic Disease
    Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinic receptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors.
  • HY-P1269A
    α-Conotoxin AuIB TFA

    nAChR Neurological Disease
    α-Conotoxin AuIB TFA, a potent and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist, blocks α3β4 nAChRs expressed in Xenopus oocytes with an IC50 of 0.75 μM.
  • HY-15790
    Elobixibat

    A 3309; AZD 7806

    Others Metabolic Disease
    Elobixibat is a potent ileal bile acid transporter (IBAT) inhibitor with IC50 values of 0.53 ± 0.17 nM, 0.13 ± 0.03 nM, and 5.8 ± 1.6 nM for human IBAT, mouse IBAT, and canine IBAT.
  • HY-12741
    LDN-212320

    LDN/OSU-0212320; LDN-0212320; OSU-0212320

    EAAT2 Neurological Disease
    LDN-212320(OSU-0212320) is a glutamate transporter EAAT2 activator; enhances EAAT2 levels by > 6 fold at concentrations < 5 μM after 24 h.
  • HY-19264
    264W94

    Others Metabolic Disease
    264W94 is a potent ileal bile acid transporter (IBAT) inhibitor and a new cholesterol lowering agent. 264W94 has CYP7A1 induction, and antilipemic action.
  • HY-111419
    DSP-1053

    Serotonin Transporter Neurological Disease
    DSP-1053 is a potent Serotonin Transporter (SERT) (Ki=1.02 nM) inhibitor with partial 5-HT1A receptor (Ki=5.05 nM) agonistic activity.
  • HY-101918
    DS-1040 Tosylate

    Others Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
  • HY-126302
    DMT1 blocker 2

    Others Inflammation/Immunology
    DMT1 blocker 2, Compound 12f, is a direct inhibitor of divalent metal transporter 1 (DMT1) with an IC50 of 0.83 μM, is expected to block iron uptake by enterocytes in vivo.
  • HY-13217
    Vanoxerine dihydrochloride

    GBR-12909 dihydrochloride; I893 dihydrochloride

    Dopamine Transporter Neurological Disease
    Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) binds to the target site on the dopamine transporter (DAT).
  • HY-13217A
    Vanoxerine

    GBR 12909; I893

    Dopamine Transporter Neurological Disease
    Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine (GBR-12909) binds to the target site on the dopamine transporter (DAT).
  • HY-12501A
    ITI-214

    Phosphodiesterase (PDE) Neurological Disease
    ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).
  • HY-122190
    TAK-071

    mAChR Neurological Disease
    TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM.
  • HY-16191
    ELR510444

    Microtubule/Tubulin Apoptosis Cancer
    ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines.
  • HY-B1700A
    Mivacurium dichloride

    nAChR Neurological Disease
    Mivacurium dichloride is a benzylisoquinoline derivative and is a short-acting non-depolarizing neuromuscular blocking agent and skeletal muscle relaxant. Mivacurium dichloride couples with the nAChR to reduce or inhibit the depolarizing effect of acetylcholine on the terminal disc of the muscle cell.
  • HY-101281A
    (Rac)-VU 6008667

    mAChR Neurological Disease
    (Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC50=1.8 μM, pIC50= 5.75), has high CNS penetration.
  • HY-125901
    D-Tubocurarine chloride pentahydrate

    nAChR Neurological Disease
    D-Tubocurarine chloride pentahydrate is the chloride salt form of Tubocurarine, a nicotinic acetylcholine receptors (AChR) antagonist, and can be used as a skeletal muscle relaxant during surgery or mechanical ventilation. D-Tubocurarine chloride pentahydrate is also a potent neuromuscular blocking agent.
  • HY-12501
    ITI214 free base

    Phosphodiesterase (PDE) Neurological Disease
    ITI-214 (free base) is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).
  • HY-N0647
    Silychristin

    Others Endocrinology
    Silychristin is an abundant flavonolignan present in the fruits of Silybum marianum, with antioxidant properties. Silychristin is a potent inhibitor of the thyroid hormone transporter MCT8, and elicits a strong inhibition of T3 uptake with an IC50 of 110 nM.
  • HY-B0486
    Lonidamine

    AF-1890; Diclondazolic Acid; DICA

    Hexokinase Mitochondrial Metabolism Apoptosis Cancer
    Lonidamine (AF-1890), an antitumor agent, is a hexokinase, mitochondrial pyruvate carrier (Ki 2.5 μM in isolated rat liver mitochondria) and plasma membrane monocarboxylate transporters inhibitor, which also inhibits mitochondrial complex II.
  • HY-P1268
    α-Conotoxin PIA

    nAChR Neurological Disease
    α-Conotoxin PIA is a nicotinic acetylcholine receptor (nAChR) antagonist isolated from Conus purpurascens that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。
  • HY-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-15084A
    (-)-Dizocilpine maleate

    (-)-MK-801 maleate

    iGluR Neurological Disease
    (-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a Ki of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects.
  • HY-B1190A
    Cefadroxil hydrate

    BL-S 578 hydrate

    Bacterial Antibiotic Infection
    Cefadroxil hydrate (BL-S 578 hydrate) is an orally active and first-generation cephalosporin with a broad spectrum antibacterial activity. Cefadroxil hydrate (BL-S 578 hydrate) also acts as a substrate of the peptide transporter PEPT1 and PEPT2.
  • HY-N0406
    2"-O-beta-L-galactopyranosylorientin

    Others Metabolic Disease
    2"-O-beta-L-galactopyranosylorientin is extracted from the flowers of Trollius ledebouri. 2"-O-beta-L-galactopyranosylorientin involves transporter mediated efflux in addition to passive diffusion and is the substrate of multidrug resistance protein 2 (MRP2).
  • HY-N6608
    Physostigmine

    Eserine

    AChE Neurological Disease
    Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and elevate acetylcholine levels in the brain. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning.
  • HY-P1268A
    α-Conotoxin PIA TFA

    nAChR Neurological Disease
    α-Conotoxin PIA TFA is a nicotinic acetylcholine receptor (nAChR) antagonist isolated from Conus purpurascens that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。
  • HY-117506
    (S)-SBFI-26

    FABP Neurological Disease
    (S)-SBFI-26 is the (S) enantiomer of SBFI-26, an anti-nociceptive agent binds to anandamide transporters FABP5 and FABP7. (S)-SBFI-26 has anti-nociceptive and anti-inflammatory effects.
  • HY-19753
    KS176

    BCRP Cancer
    KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter (IC50 values are 0.59 and 1.39 μM in Pheo A and Hoechst 33342 assays respectively). Displays no inhibitory activity against P-gp or MRP1.
  • HY-124658
    G0507

    Bacterial Infection
    G0507, a pyrrolopyrimidinedione compound, is a potent LolCDE ABC Transporter inhibitor. G0507 is a inhibitor of Escherichia coli growth and induces the extracytoplasmic σE stress response. G0507 acts as a chemical probe to dissect lipoprotein trafficking in Gram-negative bacteria.
  • HY-10936
    S 18986

    iGluR Neurological Disease
    S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests.
  • HY-106901A
    Asoxime dichloride

    HI-6

    nAChR Neurological Disease
    Asoxime dichloride (HI-6) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride involves in modulating immunity response. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system.
  • HY-108540
    LAT1-IN-1

    BCH

    Apoptosis Cancer
    LAT1-IN-1 (BCH) is a selective and competitive inhibitor of large neutral amino acid transporter 1 (LAT1) significantly inhibit cellular uptake of amino acids and mTOR phosphorylation, which induces the suppression of cancer growth and apoptosis.
  • HY-D0067
    7ACC1

    DEAC; Coumarin D 1421; D 1421

    Monocarboxylate Transporter Cancer
    7ACC1(DEAC; Coumarin D 1421; D 1421) selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.
  • HY-15793A
    Trans (2,3)-Dihydrotetrabenazine

    (2R,3R,11bR)-rel-Dihydrotetrabenazine; (2R,3R,11bR)-rel-DHTBZ

    Drug Metabolite Monoamine Transporter Neurological Disease
    Trans (2,3)-Dihydrotetrabenazine ((2R,3R,11bR)-rel-Dihydrotetrabenazine), a metabolite of Tetrabenazine, shows remarkable inhibition activity on vesicular monoamine transporter (VMAT2).
  • HY-114395
    NVS-ZP7-4

    Others Inflammation/Immunology
    NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
  • HY-N6936
    Sennidin A

    HCV Akt GLUT Infection
    Sennidin A, isolated from the leaves of Cassia angustifolia, inhibits HCV NS3 helicase, with an IC50 of 0.8 μM. Sennidin A induces phosphorylation of Akt and glucose transporter 4 (GLUT4) translocation. Sennidin A stimulates the glucose incorporation.
  • HY-B2155
    Acotiamide monohydrochloride trihydrate

    AChE Metabolic Disease
    Acotiamide monohydrochloride trihydrate is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia. Acotiamide monohydrochloride trihydrate enhances acetylcholine released by enteric neurons through muscarinic receptor antagonism and acetylcholinesterase (AChE) inhibition, thereby enhancing gastric emptying and gastric accommodation.
  • HY-100228A
    SKF89976A hydrochloride

    d,l-SKF89976A hydrochloride

    GABA Receptor Neurological Disease
    SKF89976A hydrochloride is a selective GABA transporter (GAT-1) inhibitor with IC50s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-W008610
    GBR 12783

    Dopamine Receptor Neurological Disease
    GBR 12783 is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 can improve memory performance and increase hippocampal acetylcholine release in rats.
  • HY-100968
    GBR 12783 dihydrochloride

    Dopamine Receptor Neurological Disease
    GBR 12783 dihydrochloride is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 dihydrochloride can improve memory performance and increase hippocampal acetylcholine release in rats.
  • HY-N4137
    Tormentic acid

    Others Inflammation/Immunology Cardiovascular Disease
    Tormentic acid, a triterpene isolated from Rosa rugosa, exerts anti-inflammatory, antihyperlipidemic, and anti-atherogenic properties.
  • HY-122312
    BAY-8002

    Monocarboxylate Transporter Cancer
    BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity.
  • HY-N2003
    D-Tetrahydropalmatine

    Dopamine Receptor Metabolic Disease
    D-Tetrahydropalmatine is an isoquinoline alkaloid, mainly in the genus Corydalis. D-Tetrahydropalmatine is a Dopamine (DA) receptor antagonist with preferential affinity toward the D1 receptors. D-Tetrahydropalmatine is a potent organic cation transporter 1 (OCT1) inhibitor.
  • HY-76772
    Cevimeline hydrochloride hemihydrate

    SNI-2011; AF102B hydrochloride hemihydrate

    mAChR Neurological Disease
    Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB).
  • HY-70020B
    Cevimeline hydrochloride

    AF102B hydrochloride

    mAChR Neurological Disease
    Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride can cross the blood-brain barrier (BBB).
  • HY-109120
    Odevixibat

    A4250

    Others Metabolic Disease
    Odevixibat (A4250) is a potent, selective and orally active inhibitor of the ileal bile acid transporter (IBAT). Odevixibat (A4250)decreases cholestatic liver and bile duct injury in mice model. Odevixibat (A4250) has the potential for the treatment of primary biliary cirrhosis.
  • HY-128974
    N-Dodecyl-β-D-maltoside

    Lauryl Maltoside

    Others Others
    N-Dodecyl-β-D-maltoside (Lauryl Maltoside) is a derivatives of pyrene (Py), and it is a alkyl maltopyranoside detergent, especially in transporters and respiratory complexes. N-Dodecyl-β-D-maltoside has also been employed in applications such as in the purification and stabilization of RNA polymerase and detection of protein-lipid interactions.
  • HY-10020
    Varenicline Hydrochloride

    CP 526555 hydrochloride

    nAChR Neurological Disease
    Varenicline Hydrochloride (CP 526555 hydrochloride) is a high affinity, selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist and full α7 nAChR agonist. Varenicline Hydrochloride is also a potent partial agonist of α6β2 nAChR in striatum of rats with a Ki value of 0.12 nM.
  • HY-70020
    Cevimeline

    AF102B

    mAChR Neurological Disease
    Cevimeline (AF-102B) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline can cross the blood-brain barrier (BBB).
  • HY-111678
    ML230

    CID44640177; SID 88095709

    Others Cancer
    ML230 (CID44640177; SID 88095709) is a selective inhibitor of ATP-binding cassette (ABC) transporter ABCG2, and 36-fold selective for ABCG2 over ABCB1 with EC50s values of 0.13 μM and 4.65 μM, respectively.
  • HY-G0025
    Tetrabenazine Metabolite

    (-)-β-Dihydrotetrabenazine; (-)-β-HTBZ

    Monoamine Transporter Drug Metabolite Neurological Disease
    Tetrabenazine Metabolite is an active metabolite of Tetrabenazine. Tetrabenazine Metabolite is a vesicular monoamine transporter 2 (VMAT2) inhibitor with a high affinity (Ki=13.4 nM). Tetrabenazine Metabolite is be developed for the treatment of chorea associated with Huntington’s disease and other hyperkinetic disorders.
  • HY-16643
    Linerixibat

    GSK2330672

    Others Metabolic Disease Inflammation/Immunology
    Linerixibat (GSK2330672) is a highly potent, nonabsorbable and orally active apical sodium-dependent bile acid transporter (ASBT) inhibitor with an IC50 of 42 nM human ASBT. Linerixibat can be used as lipid-lowering agent. Linerixibat has the potential for type 2 diabetes and Primary Biliary Cholangitis treatment.
  • HY-125176
    G907

    Bacterial Infection
    G907 is a selective small-molecule antagonist of ATP-binding cassette (ABC) transporter, MsbA. It inhibits purified E. coli MsbA in amphipols with an IC50 of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket. Bactericidal activity.
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-B0590B
    (+)-Tetrabenazine

    (+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine

    Monoamine Transporter Cancer
    (+)-Tetrabenazine ((+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine) is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2), inhibits transport by VMAT2 with 10-fold greater potency than transport by VMAT1.
  • HY-N6935
    Sennidin B

    HCV Akt GLUT Infection Metabolic Disease
    Sennidin B, a stereoisomer isolated from the leaves of Cassia angustifolia, has lower activity than Sennidin A. Sennidin A inhibits HCV NS3 helicase, with an IC50 of 0.8 μM. Sennidin A induces phosphorylation of Akt and glucose transporter 4 (GLUT4) translocation. Sennidin A stimulates the glucose incorporation .
  • HY-P1365
    α-Conotoxin MII

    α-CTxMII

    nAChR Neurological Disease
    α-Conotoxin MII (α-CTxMII), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII (α-CTxMII) potently blocks β3-containing neuronal nicotinic receptors .
  • HY-107676
    SIB-1553A

    nAChR Neurological Disease
    SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders.
  • HY-103430
    SKF-83566 hydrobromide

    Dopamine Receptor Neurological Disease
    SKF-83566 hydrobromide is a potent, blood-brain permeable and orally active dopamine D1/D5 receptor antagonist. SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM and attenuates cocaine effects in vivo.
  • HY-N0749
    Jatrorrhizine

    Others Neurological Disease
    Jatrorrhizine is a potent and orally active uptake-2 transporter inhibitor, it can be isolated from various Chinese medicinal plants. Jatrorrhizine exhibits a critical neuroprotective role in H2O2-induced apoptosis via inhibition of MAPK pathway in HT22 hippocampal neurons.
  • HY-N0740
    Jatrorrhizine chloride

    Others Neurological Disease
    Jatrorrhizine chloride is a potent and orally active uptake-2 transporter inhibitor, it can be isolated from various Chinese medicinal plants. Jatrorrhizine chloride exhibits a critical neuroprotective role in H2O2-induced apoptosis via inhibition of MAPK pathway in HT22 hippocampal neurons.
  • HY-10019
    Varenicline

    CP 526555

    nAChR Neurological Disease
    Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment.
  • HY-P1365A
    α-Conotoxin MII TFA

    α-CTxMII TFA

    nAChR Neurological Disease
    α-Conotoxin MII TFA (α-CTxMII TFA), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII TFA (α-CTxMII TFA) potently blocks β3-containing neuronal nicotinic receptors .
  • HY-N0801
    Polygalacic acid

    MMP AChE Inflammation/Immunology Neurological Disease
    Polygalacic acid, is a triterpene, isolated from the root of Polygala tenuifolia Willd. Polygalacic acid inhibits MMP expression. Polygalacic acid may have a therapeutic effect in Osteoarthritis (OA) treatment . Polygalacic acid exerts a significant neuroprotective effect on cognitive impairment, PA improves cholinergic system reactivity by inhibiting acetylcholinesterase (AChE) activity, increasing choline acetyltransferase (ChAT) activity, and elevating levels of acetylcholine (Ach) in the hippocampus and frontal cortex.
  • HY-135482
    GABAA receptor agent 2 TFA

    GABA Receptor Neurological Disease
    GABAA receptor agent 2 TFA is a potent and high-affinity GABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2 GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3).
  • HY-117203A
    CDK12-IN-E9

    CDK Cancer
    CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM.
  • HY-114395A
    (R)-NVS-ZP7-4

    Others Inflammation/Immunology
    (R)-NVS-ZP7-4 is the R-isomer of NVS-ZP7-4. NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
  • HY-N0755
    Rhoifolin

    Insulin Receptor GLUT NF-κB p38 MAPK Autophagy Metabolic Disease Endocrinology Cancer
    Rhoifolin is a flavone glycoside isolated from Citrus grandis (L.) Osbeck leaves. Rhoifolin is beneficial for diabetic complications through enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and glucose transporter 4 (GLUT 4) translocation. Rhoifolin ameliorates titanium particle-stimulated osteolysis and attenuates osteoclastogenesis via RANKL-induced NF-κB and MAPK pathways.
  • HY-W008344
    2-Chloroadenosine

    Others Others
    2-Chloroadenosine, a stable adenosine analogue, protects against long term development of ischaemic cell loss in the rat hippocampus. 2-Chloroadenosine is an apparent competitive inhibitor of uridine influx (apparent Ki=33 μM) and high-affinity nitrobenzylthioinosine binding (apparent Ki=0.18 mM). 2-Chloroadenosine is a transported permeant for the nucleoside transporter in human erythrocytes.
  • HY-N0173
    Cinchonidine

    α-Quinidine

    Serotonin Transporter Parasite Infection
    Cinchonidine (α-Quinidine) is a cinchona alkaloid found in Cinchona officinalis and Gongronema latifolium. A building block used in asymmetric synthesis in organic chemistry. Weak inhibitor of serotonin transporter (SERT) with Kis of 330, 4.2, 36, 196, 15 μM for dSERT, hSERT, hSERT I172M, hSERT S438T, hSERT Y95F, respectively. Antimalarial activities.
  • HY-100619
    BMS-986020

    LPL Receptor Metabolic Disease Inflammation/Immunology
    BMS-986020 is a high-affinity and selective lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively. BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).
  • HY-100619A
    BMS-986020 sodium

    LPL Receptor Metabolic Disease Inflammation/Immunology
    BMS-986020 sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 sodium inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively. BMS-986020 sodium has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).
  • HY-116594A
    OPC-14523 hydrochloride

    Sigma Receptor 5-HT Receptor Neurological Disease
    OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity.
  • HY-109067
    Opiranserin

    GlyT 5-HT Receptor P2X Receptor Neurological Disease
    Opiranserin, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain.
  • HY-14565
    Pozanicline

    ABT-089

    nAChR Neurological Disease
    Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [ 3H] cytisine sites is 16.7 nM. Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction.
  • HY-133011
    nAChR agonist 1

    nAChR Neurological Disease
    nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca 2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease.
  • HY-111191
    ONO-2952

    Others Neurological Disease
    ONO-2952 is a potent, selective and orally active translocator protein 18 kDa (TSPO) antagonist with Ki of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes. ONO-2952 exerts its anti-stress effects through inhibition of excessive activation of noradrenergic system in the brain without the amnesic effect. ONO-2952 has the potential for irritable bowel syndrome treatment.
  • HY-13779
    J-147

    Monoamine Oxidase Dopamine Transporter Neurological Disease
    J-147 is an exceptionally potent, orally active, neuroprotective agent for cognitive enhancement. J-147 can readily pass the blood brain barrier (BBB). J-147 can inhibit monoamine oxidase B (MAO B) and the dopamine transporter with EC50 values of 1.88 μM and 0.649 μM, respectively. J-147 has potential for the treatment of Alzheimer’s disease (AD).
  • HY-116594
    OPC-14523 free base

    Sigma Receptor 5-HT Receptor Neurological Disease
    OPC-14523 free base is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 free base shows antidepressant-like activity.
  • HY-122872
    MKK7-COV-9

    p38 MAPK Cancer
    MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
  • HY-120184
    VU0467485

    AZ13713945

    mAChR Neurological Disease
    VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity.
  • HY-125990
    SLC13A5-IN-1

    Sodium Channel Metabolic Disease Cardiovascular Disease
    SLC13A5-IN-1 is a selective sodium-citrate co-transporter (SLC13A5) inhibitor. SLC13A5-IN-1 completely blocks the uptake of  14C-citrate with an IC50 value of 0.022 μM in HepG2 cells. SLC13A5-IN-1 has the potential for the treatment of metabolic and/or cardiovascular diseases. SLC13A5-IN-1 is extracted from patent WO2018104220A1, Compound I-5.
  • HY-124619
    GPI-1046

    FKBP HIV Infection Neurological Disease
    GPI-1046 is a immunophilin ligand without antibiotic action and attenuates ethanol intake in part through the upregulation of glutamate transporter 1 (GLT1) in PFC and NAc-core. GPI-1046 is an analog of FK506, which is an immunophilin ligand that has been shown neuroprotective effects in neurodegenerative disease models. GPI-1046 readily crosses the blood-brain barrier and promotes the regeneration of dopamine (DA) cells in the CNS in association with functional recovery in rodent models. GPI-1046 improves HIV-associated injury of peripheral nerves.
  • HY-15310
    Ivermectin

    MK-933

    Parasite HIV Mitophagy HSV SARS-CoV Antibiotic Autophagy Infection Cancer
    Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.
  • HY-120944
    BAY-7598

    MMP Inflammation/Immunology
    BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.